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C7280948 is a sulfone inhibitor of PRMT1 (IC50 values 12.75 μM and 26.7 μM, respectively, methylated substrates for oligopeptides containing human histone H4 and non-histone Npl3 1-21 amino acids). PRMT inhibitors are a potential compound and interesting tool for cell biology. C7280948 is an effective tool for studying the epigenetic effects of PRMT1. PRMT1 is also involved in activation of estrogen and androgen receptors. PRMT1 is an essential component of the oncogenic transformation induced by the mixed line leukemia (MLL) complex, and thus may represent a new research direction in hormone-dependent cancers.
| Molecular Weight | 276.35 |
| Formula | C14H16N2O2S |
| CAS Number | 587850-67-7 |
| Solubility (25°C) | DMSO 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PRMTs Products |
|---|
| EPZ015666
EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
| SGC707
SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively. |
| EPZ020411
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8. |
| XY1
XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive. |
| SGC2085
SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. |
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